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Double-layer moxifloxacin suppository and preparation method thereof

A moxifloxacin hydrochloride, double-layer technology, applied in the field of double-layer suppositories, can solve the problems of not showing the superiority of suppositories, and achieve the effects of avoiding toxic and side effects, good curative effect and long duration

Inactive Publication Date: 2011-04-13
北京化药科创医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This document only reports the preparation method and quality control of ordinary suppositories. Although it is a topical dosage form developed for the clinical use of moxifloxacin in the treatment of genitourinary tract infections, the dissolution rate and bioavailability of the dosage form are not carried out. The screening of other tests does not reflect the superiority of suppositories

Method used

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  • Double-layer moxifloxacin suppository and preparation method thereof
  • Double-layer moxifloxacin suppository and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Preparation of moxifloxacin double-layer suppository: preparation of the slow-release part Take the water-soluble matrix of 135g of gelatin and 75g of glycerin, heat and melt in a water bath, add 12g of moxifloxacin hydrochloride under stirring, mix well, and pour it into the vaginal suppository while heating In the mold, cool, demould, and set aside; preparation of the quick-release part Take an appropriate amount of PEG 1000156g, PEG 40008g, water 18ml, glycerin 10g, heat and melt in a water bath, add 8g of moxifloxacin hydrochloride under stirring, mix well and multiply Pour the heat into the vaginal suppository mold, and after cooling down slightly, insert the prepared sustained-release suppository to the end (try to insert from the center), and it is ready. Each suppository contains 200 mg of moxifloxacin hydrochloride.

Embodiment 2

[0023] In Vitro Dissolution Determination: Comparison of In Vitro Dissolution of Double-layer Suppositories and Common Suppositories (1) In Vitro Dissolution Determination of Double-layer Suppositories: Using the Rotating Basket Method, Take a Moxifloxacin Double-Layer Suppository in Example 1 and Place It in Stainless Steel In the mesh basket, the outer surface is covered with a 0.8um microporous filter membrane to form a cylinder, and then the cylinder is placed in the rotating basket. The dissolution medium is 900ml of artificial intestinal fluid, the temperature is (37.5±0.1)°C, and the rotation speed is 150r / min. Regularly sample 5ml, filter (replenish medium 5ml immediately after each sampling), discard the primary filtrate, accurately measure 4ml of the subsequent filtrate, put it in a 10ml volumetric flask, add artificial intestinal juice to the scale, and measure the absorption at a wavelength of 296nm with the dissolution medium as a blank Degree A, calculate the medi...

Embodiment 3

[0025] Stimulation test: 6 healthy adult rabbits were taken, weighing (3.0±0.5) kg, and the rabbits were divided into two groups, namely the drug treatment group and the blank control group. The moxifloxacin double-layer suppository in Example 1 and the excipient with the same matrix but without moxifloxacin were placed into the rectum of the rabbit, administered once every other day for 8 days, and killed 48 hours after the last administration , Take out the local mucous membrane, observe that there is no hyperemia and redness in the medication group, and the observation results are no different from those in the blank control group.

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Abstract

The invention discloses a double-layer moxifloxacin suppository and a preparation method thereof, which aim to provide a locally-applied suppository with quick response, good curative effect, nonirritant and minimal side effect. The double-layer suppository is divided into an inner layer and an outer layer, wherein the outer layer is a quick-release part which is quickly released to quickly reach optimal blood concentration; and the inner layer is a sustained-release part which is actually an ordinary-release part not subjected to sustained-release treatment. The double-layer moxifloxacin suppository is applied from the vagina so as to avoid the damages of first pass effect of the liver to oral medication and the toxic or side effect of systemic administration, and make the effective medicament concentration of a local lesion greatly exceed levels obtained by oral medication and injection, has long effective duration and the curative effect remarkably better than that of the systemic administration, and is applied to the treatment of vaginitis caused by the infections of staphylococcus aureus, Chlamydia and the like.

Description

technical field [0001] The invention relates to a double-layer suppository containing moxifloxacin, its salt and / or hydrate, its preparation method and the application of the preparation in preventing and treating women's reproductive tract infection. Background technique [0002] As the fourth-generation quinolone antibacterial drug, Moxifloxacin not only maintains the advantages of the third-generation quinolones, such as wide antibacterial spectrum, strong antibacterial activity, and good tissue penetration, but also further expands the antibacterial spectrum to pathogens such as chlamydia and mycoplasma, and is effective against Gram-positive bacteria and anaerobic bacteria were significantly stronger than the third generation. The antibacterial mechanism of the drug is to interfere with II and IV topoisomerases. [0003] Currently, moxifloxacin is available in the form of tablets and injections (manufactured by Bayer, Germany), and has applied for patents in China for ...

Claims

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Application Information

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IPC IPC(8): A61K9/02A61K31/4709A61K47/34A61K47/42A61K47/10A61J3/08A61P13/00A61P15/00A61P15/02A61P31/04
Inventor 关屹闫冬
Owner 北京化药科创医药科技发展有限公司
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